发明名称 Indole-1-carboxamides as kinase inhibitors
摘要 This invention is directed to a compound of Formula I; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, and X are as defined herein. The compounds of Formula I are useful as receptor tyrosine kinase (RTK) inhibitors and can be used to treat such diseases as cancer, blood vessel proliferative disorders, fibrotic disorders, mesangial cell proliferative disorders and metabolic diseases.
申请公布号 US9353093(B2) 申请公布日期 2016.05.31
申请号 US201414509007 申请日期 2014.10.07
申请人 Allergan, Inc. 发明人 Boral Sougato;Malone Thomas C.;Wang Shimiao
分类号 C07D209/04;C07D409/14;C07D209/26;C07D405/12;C07D409/04 主分类号 C07D209/04
代理机构 代理人 Bass Jonathan
主权项 1. A compound represented by Formula I or an enatiomer, diastereoisomer or pharmaceutically acceptable salt thereof:wherein: R1 is substituted or unsubstituted heterocycle or substituted or unsubstituted aryl; X is R2 is substituted or unsubstituted heterocycle or substituted or unsubstituted aryl; R3 is hydrogen, substituted or unsubstituted C1-C8 alkyl, substituted or unsubstituted heterocycle, substituted or unsubstituted aryl, halogen, hydrogen, (CR8R9)aC(O)OR10, (CR8R9)aOR10, (CR8R9)aN(R11)C(O)OR10, (CR8R9)aC(O) N(R11R12)2, (CR8R9)aN(R11)C(O)OR10, (CR8R9)aN(R11)C(O)N(R11R12)2 or (CR8R9)aN(R11R12)2; R4 is hydrogen, substituted or unsubstituted C1-C8 alkyl, substituted or unsubstituted heterocycle, substituted or unsubstituted aryl, halogen, hydrogen, (CR8R9)aC(O)OR10, (CR8R9)aOR10, (CR8R9)aN(R11)C(O)OR10, (CR8R9)aC(O) N(R11R12)2, (CR8R9)aN(R11)C(O)OR10, (CR8R9)aN(R11)C(O)N(R11R121)2 or (CR8R9)aN(R11R12)2; R5 is hydrogen, substituted or unsubstituted C1-C8 alkyl, substituted or unsubstituted heterocycle, substituted or unsubstituted aryl, halogen, hydrogen, (CR8R9)aC(O)OR10, (CR8R9)aOR10, (CR8R9)aN(R11)C(O)OR10, (CR8R9)aC(O) N(R11R121)2, (CR8R9)aN(R11)C(O)OR10, (CR8R9)aN(R11)C(O)N(R11R12)2 or (CR8R9)aN(R11R12)2; R6 is hydrogen, substituted or unsubstituted C1-C8 alkyl, substituted or unsubstituted heterocycle, substituted or unsubstituted aryl, halogen, hydrogen, (CR8R9)aC(O)OR10, (CR8R9)aOR10, (CR8R9)aN(R11)C(O)OR10, (CR8R9)aC(O)N(R11R121)2, (CR8R9)aN(R11)C(O)OR10, (CR8R9)aN(R11)C(O)N(R11R12)2 or (CR8R9)aN(R11R12)2; R7 is hydrogen, substituted or unsubstituted C1-C8 alkyl, substituted or unsubstituted heterocycle, substituted or unsubstituted aryl, halogen, hydrogen, (CR8R9)aC(O)OR10, (CR8R9)aOR10, (CR8R9)aN(R11)C(O)OR10, (CR8R9)aC(O)N(R11R121)2, (CR8R9)aN(R11)C(O)OR10, (CR8R9)aN(R11)C(O)N(R11R12)2 or (CR8R9)aN(R11R12)2; R8 is substituted or unsubstituted C1-8 alkyl, hydrogen, fluoro, —CH2OH, —OH, COCH3, CH2CH2OH, CH2CH2CH2OH or CH2CH2OCH2CH2OH; R9 is substituted or unsubstituted C1-8 alkyl, hydrogen, fluoro or —OH; R10 is substituted or unsubstituted C1-8 alkyl or hydrogen; R11 is substituted or unsubstituted C1-8 alkyl, hydrogen or can form together with the N and R12 a substituted or unsubstituted heterocycle; R12 is substituted or unsubstituted C1-8 alkyl, hydrogen or can form together with the N and R11 a substituted or unsubstituted heterocycle; and a is 0, 1, 2, 3 or 4.
地址 Irvine CA US